Direct site-specific radiolabeling of an Affibody protein with 4-[18F]fluorobenzaldehyde via oxime chemistry.

Autor: Mohammad Namavari, Omayra Padilla De Jesus, Zhen Cheng, Abhijit De, Ernest Kovacs, Jelena Levi, Rong Zhang, Joshua Hoerner, Hans Grade, Faisal Syud, Sanjiv Gambhir, Namavari, Mohammad, Padilla De Jesus, Omayra, Cheng, Zhen, De, Abhijit, Kovacs, Ernest, Levi, Jelena, Zhang, Rong, Hoerner, Joshua K, Grade, Hans
Předmět:
Zdroj: Molecular Imaging & Biology; Jul2008, Vol. 10 Issue 4, p177-181, 5p
Abstrakt: Purpose: In this study, we introduce a methodology for preparing 18F-labeled Affibody protein, specifically 18F-Anti-HER2 dimeric Affibody (14 kDa), for in vivo imaging of HER2neu with positron emission tomography (PET).Procedures: We have used 4-[18F]fluorobenzaldehyde as a synthon to prepare 18F-Anti-HER2 Affibody. Aminooxy-functionalized Affibody (Anti-HER2-ONH2) was incubated with 4-[18F]fluorobenzaldehyde in ammonium acetate buffer at pH 4 in the presence of methanol at 70 degrees C for 15 min. The resulting 18F-labeled Affibody molecule was evaluated as a PET probe in xenograft models expressing HER2.Results: We have successfully prepared 18F-Anti-HER2 dimeric Affibody (14 kDa), N-(4-[18F]fluorobenzylidine)oxime-Anti-HER2 Affibody, [18F]FBO-Anti-HER2, in 26-30% radiochemical yields (decay corrected). High-contrast small-animal PET images with relatively moderate tumor uptake (1.79 +/- 0.40% ID/g) were observed for the 18F-Anti-HER2 Affibody.Conclusion: Site-specific 18F-labeled Affibody against HER2 has been synthesized via chemoselective oxime formation between an aminooxy-functionalized Affibody and 18F-fluorobenzaldehyde. The results have implications for radiolabeling of other affibodies and macromolecules and should also be important for advancing Affibody imaging with PET. [ABSTRACT FROM AUTHOR]
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